Srikumar R, Kon T, Gotoh N, Poole K
Department of Microbiology and Immunology, Queen's University, Kingston, Ontario, Canada.
Antimicrob Agents Chemother. 1998 Jan;42(1):65-71. doi: 10.1128/AAC.42.1.65.
The mexCD-oprJ and mexAB-oprM operons encode components of two distinct multidrug efflux pumps in Pseudomonas aeruginosa. To assess the contribution of individual components to antibiotic resistance and substrate specificity, these operons and their component genes were cloned and expressed in Escherichia coli. Western immunoblotting confirmed expression of the P. aeruginosa efflux pump components in E. coli strains expressing and deficient in the endogenous multidrug efflux system (AcrAB), although only the delta acrAB strain, KZM120, demonstrated increased resistance to antibiotics in the presence of the P. aeruginosa efflux genes. E. coli KZM120 expressing MexAB-OprM showed increased resistance to quinolones, chloramphenicol, erythromycin, azithromycin, sodium dodecyl sulfate (SDS), crystal violet, novobiocin, and, significantly, several beta-lactams, which is reminiscent of the operation of this pump in P. aeruginosa. This confirmed previous suggestions that MexAB-OprM provides a direct contribution to beta-lactam resistance via the efflux of this group of antibiotics. An increase in antibiotic resistance, however, was not observed when MexAB or OprM alone was expressed in KZM120. Thus, despite the fact that beta-lactams act within the periplasm, OprM alone is insufficient to provide resistance to these agents. E. coli KZM120 expressing MexCD-OprJ also showed increased resistance to quinolones, chloramphenicol, macrolides, SDS, and crystal violet, though not to most beta-lactams or novobiocin, again somewhat reminiscent of the antibiotic resistance profile of MexCD-OprJ-expressing strains of P. aeruginosa. Surprisingly, E. coli KZM120 expressing MexCD alone also showed an increase in resistance to these agents, while an OprJ-expressing KZM120 failed to demonstrate any increase in antibiotic resistance. MexCD-mediated resistance, however, was absent in a tolC mutant of KZM120, indicating that MexCD functions in KZM120 in conjunction with TolC, the previously identified outer membrane component of the AcrAB-TolC efflux system. These data confirm that a tripartite efflux pump is necessary for the efflux of all substrate antibiotics and that the P. aeruginosa multidrug efflux pumps are functional and retain their substrate specificity in E. coli.
mexCD-oprJ和mexAB-oprM操纵子编码铜绿假单胞菌中两种不同的多药外排泵的组成部分。为了评估各个组成部分对抗生素耐药性和底物特异性的贡献,将这些操纵子及其组成基因克隆并在大肠杆菌中表达。蛋白质免疫印迹法证实了在表达和缺乏内源性多药外排系统(AcrAB)的大肠杆菌菌株中铜绿假单胞菌外排泵组成部分的表达,尽管只有ΔacrAB菌株KZM120在存在铜绿假单胞菌外排基因的情况下对抗生素的耐药性有所增加。表达MexAB-OprM的大肠杆菌KZM120对喹诺酮类、氯霉素、红霉素、阿奇霉素、十二烷基硫酸钠(SDS)、结晶紫、新生霉素以及几种β-内酰胺类抗生素的耐药性增加,这让人联想到该泵在铜绿假单胞菌中的作用。这证实了之前的推测,即MexAB-OprM通过排出这组抗生素直接导致β-内酰胺类耐药性。然而,当单独在KZM120中表达MexAB或OprM时,未观察到抗生素耐药性增加。因此,尽管β-内酰胺类在周质中起作用,但单独的OprM不足以赋予对这些药物的耐药性。表达MexCD-OprJ的大肠杆菌KZM120对喹诺酮类、氯霉素、大环内酯类、SDS和结晶紫的耐药性也增加,尽管对大多数β-内酰胺类或新生霉素没有增加,这再次有点类似于表达MexCD-OprJ的铜绿假单胞菌菌株的抗生素耐药谱。令人惊讶的是,单独表达MexCD的大肠杆菌KZM120对这些药物的耐药性也增加,而表达OprJ的KZM120未显示出抗生素耐药性的任何增加。然而,MexCD介导的耐药性在KZM120的tolC突变体中不存在,这表明MexCD在KZM120中与TolC共同发挥作用,TolC是先前确定的AcrAB-TolC外排系统的外膜组成部分。这些数据证实,三方外排泵对于所有底物抗生素的外排是必需的,并且铜绿假单胞菌的多药外排泵在大肠杆菌中具有功能并保留其底物特异性。